In this E-Learning module, the author describes what is meant by “targeting the epigenome”. At least 700 proteins are thought to be involved in regulating/reading post-translational modifications; many of these have been discovered to bear mutations in cancer and many are considered targets for anticancer drugs development.
In this module, the author provides classification of critical epigenetic regulators divided into writers, erasers, readers, movers and shapers. Critical epigenetic regulators are often altered or mutated in cancer and thus represent targets for anticancer therapy. Besides providing details of underlining processes in terms of epigenetic regulation, the author illustrates the content with examples in particular tumour types, findings from clinical studies, current drug approvals, and perspective of drugs in development.
DNA methyltransferase (DNMT) inhibitors and histone deacetylase (HDAC) inhibitors have already entered in the clinical use. Most activity to date is seen in haematological or lymphoid malignancies. Further work is needed to translate findings to use in solid tumours.
This E-Learning module presents the current epigenetics drugs portfolio for a number of agents in preclinical, phase I, II and III development and already approved indications. The author also asks some questions, e.g. if there are 700 epigenes, how many of them are critical in cancer or how many agents in development do we really need for the same target?
Numerous reports have shown that various components of the immune response are upregulated after DNMT and/or HDAC inhibition. By providing a basic understanding on how epigenetic agents by upregulating components of the immune response may potentially enhance immunotherapy, the author opens up a wider role in the immunotherapy field.
